AR056004A1 - Derivados de pirrolo[2, 3 -d]pirimidina, metodos de sintesis de los mismos y sus intermediarios de preparacion - Google Patents

Derivados de pirrolo[2, 3 -d]pirimidina, metodos de sintesis de los mismos y sus intermediarios de preparacion

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Publication number
AR056004A1
AR056004A1 ARP060103254A ARP060103254A AR056004A1 AR 056004 A1 AR056004 A1 AR 056004A1 AR P060103254 A ARP060103254 A AR P060103254A AR P060103254 A ARP060103254 A AR P060103254A AR 056004 A1 AR056004 A1 AR 056004A1
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Argentina
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formula
alkyl
temperature
group
compound
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ARP060103254A
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English (en)
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Pfizer Prod Inc
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Publication of AR056004A1 publication Critical patent/AR056004A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56—Nitrogen atoms
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

Procedimientos e intermediarios utiles para la síntesis de compuestos pirrolo[2,3-d]pirimidina. Reivindicacion 1: Un procedimiento de preparacion de un compuesto de la formula (4a) que comprende acoplar un compuesto activado de pirrolopirimidina de la formula (2a) en la que L1 es un grupo saliente y X1 es un grupo activador, con una amina de la formula (3a), o una sal de la misma en la que R1 es alquilo C1-6; a es un numero entero entre 0 y 4; R2 es H o alquilo C1-6 y P es un grupo protector de N; en presencia de una base produciendo un producto acoplado de formula (4a). Reivindicacion 18: Un compuesto de formula (4b). Reivindicacion 19: Un procedimiento de preparacion de un compuesto de formula (4b) que comprende acoplar un compuesto de pirrolopirimidina activado de formula (2b) en la que L1 es un grupo saliente y X2 es un grupo activador, con una amina de la formula (3a), o una sal de la misma en la que R1 es alquilo C1-6; a es un numero entero entre 0 y 4; R2 es H o alquilo C1- 6 y P es un grupo protector de N; en presencia de una base. Reivindicacion 34: Un compuesto de formula (5). reivindicacion 35: Un procedimiento para la síntesis de 2,4-dicloro-7H-pirrolo[2,3-d]pirimidina que comprende las etapas de: a) hacer reaccionar 7H-pirrolo[2,3-d]pirimidina-2,4-diol con oxicloruro de fosforo en un disolvente aromático, formando una primera solucion a una primera temperatura; b) incrementar dicha primera temperatura de la primera solucion hasta una segunda temperatura; c) anadir a dicha primera solucion a la segunda temperatura una base de amna terciaria formando una segunda solucion a la segunda temperatura e; d) incrementar dicha segunda temperatura de la segunda solucion a una tercera temperatura, durante un primer intervalo de tiempo, en el que el oxicloruro de fosforo está presente entre aproximadamente 1,5 y aproximadamente 6 equivalentes y la base de amina terciaria está presente entre aproximadamente 1,0 y aproximadamente 8,0 equivalentes; ambos con relacion al 7H-pirrolo[2,3-d]pirimidina-2,4-diol de partida. Reivindicacion 38: Un procedimiento de produccion de piperidinas enriquecidas enantioméricamente de la formula (10c) en la que R1 es alquilo C1-6; a es un numero entero entre 0 y 4; R2 es H o alquilo C1-6; y Rö se elige independientemente entre el grupo constituido por H, alquilo C1-6, y grupos CF3; b es un numero entero entre 0 y 4; que comprende las etapas de a) hidrogenar asimétricamente una sal de bencil piridinio de la formula (10d) en la que X- se selecciona entre el grupo constituido por Cl, Br, F, I, triflato, tosilato y -BF4, y R'ö es alquilo C1-6, con un catalizador de rodio, iridio o rutenio y un ligando fosfina quiral en presencia de H o una fuente de H. Reivindicacion 44: Un procedimiento de produccion de piperidinas enriquecidas enantioméricamente de la formula (10c) en la que R1 es alquilo C1-6; R2 es H o alquilo C1-6; y Rö se elige entre el grupo constituido por H, alquilo C1-6 y grupos CF3; b es un numero entero entre 0 y 4; que comprende las etapas de: a) hidrogenar asimétricamente una tetrahidropiridina de la formula (10h) en la que R'ö es alquilo C1-6; con un catalizador de rodio, iridio o rutenio y un ligando fosfina quiral en presencia de H o una fuente de H.
ARP060103254A 2005-07-29 2006-07-27 Derivados de pirrolo[2, 3 -d]pirimidina, metodos de sintesis de los mismos y sus intermediarios de preparacion AR056004A1 (es)

Applications Claiming Priority (1)

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US70401105P 2005-07-29 2005-07-29

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Country Status (24)

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US (2) US8232394B2 (es)
EP (1) EP1913000B1 (es)
JP (1) JP4052523B2 (es)
KR (1) KR100987870B1 (es)
CN (1) CN101233138A (es)
AR (1) AR056004A1 (es)
AT (1) ATE540952T1 (es)
AU (1) AU2006273762A1 (es)
BR (1) BRPI0613876A2 (es)
CA (1) CA2614907C (es)
CY (1) CY1112319T1 (es)
DK (1) DK1913000T3 (es)
ES (1) ES2377771T3 (es)
IL (1) IL188372A0 (es)
MX (1) MX2008001334A (es)
NZ (1) NZ565363A (es)
PL (1) PL1913000T3 (es)
PT (1) PT1913000E (es)
RU (1) RU2384583C2 (es)
SG (1) SG170783A1 (es)
SI (1) SI1913000T1 (es)
TW (1) TWI319402B (es)
WO (1) WO2007012953A2 (es)
ZA (1) ZA200800284B (es)

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